New thiophene-1,2,4-triazole-5(3)-ones: Highly bioactive thiosemicarbazides, structures of Schiff bases and triazole–thiols

An Update of the Use of Thiocarbohydrazides and Thiosemicarbazides in the Preparation of Heterocycles and Their Biological Importance

“…Similarly, 1‐(2‐(4‐amino‐5‐oxo‐3‐(thiophene‐2‐yl‐methyl)‐4,5‐dihydro‐1,2,4‐triazole‐1‐yl)acetyl)‐4‐(4‐aryl)‐thiosemicarbazides 77a – d were synthetized via the reaction of 2‐(4‐amino‐5‐oxo‐3‐(thiophene‐2‐ylmethyl)‐4,5‐dihydro‐1,2,4‐triazol‐1‐yl)acetohydrazide ( 76 ) with aryl isothiocyanates 52a , b , w , x (Scheme ) .…”

“…When 1‐(2‐(4‐amino‐5‐oxo‐3‐(thiophene‐2‐ylmethyl)‐4,5‐dihydro‐1,2,4‐triazole‐1‐yl)acetyl)‐4‐(4‐aryl)thiosemicarbazides 77a – d were heated under reflux in basic media (NaOH), 4‐amino‐2‐((4‐(4‐aryl)‐5‐mercapto‐4 H ‐1,2,4‐triazole‐3‐yl)methyl)‐5‐(thiophene‐2‐ylmethyl)‐2 H ‐1,2,4‐triazole‐3(4 H )‐ones 142a – d were obtained in 80–90% yields (Scheme ) .…”

Synthesis of new 1,2,4-triazole compounds containing Schiff and Mannich bases (morpholine) with antioxidant and antimicrobial activities

“…The starting compound (1) was synthesized according to published literature 17 . The reaction of compound 1 and carbon disulfide in presence of potassium hydroxide gave compound 2 in high yield (Scheme 1).…”

“…Hybrid 1,2,4-triazole and 1,3,4-oxadiazole compounds are new classes of azole anti-mycobacterials, which are proved to be highly active both in vitro and in vivo 11 . Schiff bases obtained from various heterocycles have a wide range of biological activities including antifungal, antibacterial, antimalarial, antimycobacterial, antimicrobial, anti-inflammatory, antiviral, cytotoxic, anticonvulsant, antiproliferative, anticancer, and antipyretic activities [12][13][14][15][16][17][18] . N-fuctionalized morpholines have diverse pharmacological activities.…”

Synthesis and Anticancer Activity of Tolmetin Thiosemicarbazides

“…Duffy and co-workers evaluated that tolmetin and other (NSAID)s have effects on increasing the cytotoxic activity of the anti-cancer drugs (3). Thiosemicarbazides, which are intermediate products of the synthesis for bioactive heterocyclic compounds, have taken attention of the researchers because of their clinical use and diverse biological activities (4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) (Fig 1). In this work, we synthesized novel ten tolmetin thiosemicarbazide derivatives (4a-j) and investigated their anticancer activity against cancer cell lines.…”